4-(2-chloroacetamido) Benzoic Acid Derivatives as Local Anesthetic Agents: Design, Synthesis, and Characterization

 

4-(2-chloroacetamido) Benzoic Acid Derivatives as Local Anesthetic Agents: Design, Synthesis, and Characterization

 Ashish A. Kanhed1, Ashok P. Mehere1, Kavita R. Pandey2, Debarshi Kar Mahapatra3*

1Department of Pharmaceutical Chemistry, Sharad Pawar College of Pharmacy, Nagpur – 440104, Maharashtra, India

2Department of Pharmaceutical Chemistry, Kamla Nehru College of Pharmacy, Nagpur – 441108, Maharashtra, India

3Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, Nagpur – 440037, Maharashtra, India

Abstract

Local anesthetic activity was investigated with an assumed hypothesis that the essential alkyl substituted nitrogen having strong ionization characteristics (pKa in basic side) generally found in local anesthetics can be replaced by amide nitrogen, having chloro methyl group attached to the carbonyl carbon of amide. In this type of arrangement, the inductive effect exerted by chlorine provided enough ionization character to amide nitrogen. Eight esters, ten amides and one imidazole derivatives of 4-(2-chloroacetamido) benzoic acid were synthesized by Fischer’s esterification, Schotten-Baumann and substitution reactions. The synthesized derivatives (A1–A18 and A.im) were characterized by various instrumental techniques.ACD Lab Suite® was used to determine various physiochemical properties of synthesized molecules. Initially, infiltration local anesthetic activity was determined by Bianchi’s method. Five compounds (A1, A2, A4, A10, and A.im) showed promising local anesthetic activity, where the comparison was made with lignocaine HCl, thus conforming assumed hypothesis. However, the studied compounds have potency lower than that of lignocaine HCl. Compounds showing promising activity with low toxicity were studied further by in-vivo rat sciatic nerve block method using increasing doses. A.im was studied for topological similarity with lignocaine HCl where it showed good local anesthetic activity and was relatively very less toxicity. The reduced toxicity of these molecules may be attributed due to the carbonyl chloro methyl side chain. Further structural advancement may be done by researchers to increase the potency of these compounds since they are relatively less toxic than lignocaine.

HTML FULL TEXT    PDF    XML 

Screening of In Vitro Antidiabetic Activity of Herbal Formulation Meshashringi

 

Poshan Kumar Sahu*, Pushpa Prasad, Amit Roy

Columbia Institute of Pharmacy, Tekari, Raipur (CG)-493111, India

Abstract

Diabetes is diagnosis by hyperglycemia due to absolute or relative deficiency of insulin. Today’s lifestyle has been changed and sharp increase in the incidence and prevalence of diabetes mellitus has been perceived. The antidiabetic drugs reduce the gastrointestinal glucose production and absorption through the inhibition of carbohydrate digesting enzymes such as α- amylase and α-glucosidase. The present study was aimed to investigate in vitro antidiabetic activity of aqueous extract of Meshashringi formulation using enzyme inhibitory assays. The Meshashringi was evaluated against α-amylase, α-glucosidase and dipeptidyl peptidase-IV (DPP-IV). The Meshashringi revealed 50% inhibitory activity for α-amylase, α-glucosidase and DPP-IVenzyme at 106.00 μg/ml, 124.91 μg/ml and 160.67 μg/ml, respectively. Consequently, the standard drug Acarbose exhibited 50% inhibitory activity for α-amylase, α-glucosidase and DPP-IVenzyme at 37.80 μg/ml, 65.06 μg/ml and 48.22 μg/ml, respectively. The Meshashringi formulation produces dose dependent antidiabetic activity.   

HTML FULL TEXT    PDF    XML 

Apigenin Naturally Occurring Flavonoids: Occurrence and Bioactivity

 

Preeti Sen*, Poshan Kumar Sahu, Ranjita Haldar, Kamlesh Kumar Sahu, Pushpa Prasad, Amit Roy

Columbia Institute of Pharmacy, Tekari, Raipur (C.G.)-493111, India

Abstract

The flavonoid, glycosides, alkaloids saponin, tannins etc represent an unusual group of structurally diverse secondary metabolites, derived from the convergence of multiple biosynthetic pathways that are widely distributed through the plant and animal kingdoms. Many of them have been discovered through bioassay-guided chemical investigations of traditional medicines, suggesting potential therapeutic significance. Apigenin is a flavonoid found in the medicinal plant and acts as source of pharmacological activities. Potential therapeutic indications are as diverse as cancer and viral infections, inflammation and immunomodulation, neurological and psychiatric conditions, and diabetes etc. In the view of their various pharmacological and biological actions, it seems to have great therapeutic potential. 

HTML FULL TEXT    PDF    XML 

Medicinal Value of Curcuma cassia roxb: An Overview

 

Bhupendra Sahu*, Rameshroo Kenwat, Shashikant Chandrakar

Columbia Institute of Pharmacy, Tekari, Raipur-493111 (C.G.), India

Abstract

Curcuma caesia is commonly known as kali haldi and it belongs to the family Zingiberaceae.  Black turmeric is an uncommon endemic as well as ethno medicinally important of South East Asia. This herb is available throughout north-east, central India, Papi Hills of East Godavari, West Godavari, and Andhra Pradesh. In the traditional system of medicine, fresh and dried rhizomes of Curcuma caesia are used in treating leucoderma, asthma, tumours, piles, bronchitis, bruises etc. Curcuma caesia has scientifically studied for various therapeutical activities like antioxidant, antibacterial, antipyretic, larvicidal, insecticidal, antimicrobial, wound healing and anti-hyperglycaemic. The present review is an effort to give a detailed survey of the literature on its, phytochemistry, traditional uses and therapeutical studies.

HTML FULL TEXT    PDF    XML 

Aqueous Ethanol Fruit Extract of Xylopia aethiopica and Xylopic Acid Exhibit Anti-inflammatory Activity Through Inhibition of the Arachidonic Acid Pathway

 

Newman Osafo1*, Robert P. Biney1,2, David D. Obiri1

1Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, College of Health Sciences, Kwame Nkrumah University of  Science and Technology, Kumasi, Ghana

2Department of Pharmacology, School of Medical Sciences, University of Cape Coast, Cape Coast, Ghana

Abstract

In the form of a decoction, X. aethiopica is traditionally employed in the treatment of bronchitis, asthma, arthritis and rheumatism in Ghana, Nigeria and Cameroon. This study establishes the inhibitory effect of X. aethiopica and its principal constituent, xylopic acid, on the arachidonic acid pathway of inflammation.Hydrogen sulphide is endogenously produced in mammalian tissues from the enzymatic activity of cystathionine β-synthase and cystathionine γ-lyase on L-cysteine. Its involvement in the local and systemic inflammatory process has been documented in animal models. Recent studies have identified its activation of phospholipase A2 as the mechanism involved in its anti-inflammatory role. We henceforth conducted this study to investigate the inhibitory role of X. aethiopica and its principal constituent xylopic acid on hydrogen sulphide-induced inflammation and eventual effect on the activation of phospholipase A2.Sodium hydrogen sulphide (NaHS) was injected into the mouse hind paw and oedema was monitored for 60 min. Paws were examined by the histological method.X. aethiopica extract (30, 100, 300 mg kg-1) suppressed the mean maximal swelling attained at 15 min to 42.58±1.66%, 42.58±1.66% and 34.91±2.39%, respectively compared to the mean inflamed control response of 61.51±3.90%. The total paw swellings induced over the 1 h were also significantly suppressed by 31.82±5.28%, 36.19±6.01%, and 31.65±5.16%, respectively. The xylopic acid (10, 30, 100 mg kg-1) suppressed the mean maximal swelling attained at 15 min to 41.75±1.24%, 40.26±1.68% and 38.26±2.52%, respectively relative to the control response while the total paw swelling was significantly suppressed by 34.08±4.49%, 38.19±4.50% and 43.40±5.09% respectively relative to the inflamed control response. Histologically, there was a significant (P < 0.0001) reduction in cytoplasmic vacuolation, inflammation, cellular degeneration, loss of tissue organisation and necrotic tissues with administration of X. aethiopica extract and xylopic acid in the inflamed paws of the mice. This study establishes that X. aethiopica extract, and xylopic acid mediate their anti-inflammatory actions in part through inhibition of hydrogen sulphide-induced inflammation and subsequently has an inhibitory role on phospholipase A2 activation.

HTML FULL TEXT    PDF    XML 

Effect of Natural Honey on Intestinal Transit in Rats

 

E. A. Alagwu , E. E. Ngwu , D. N. Alagwu , G. C. Uloneme*

Departments of Physiology and Anatomy, College of Medicine, Imo State University, Owerri- 460222, Nigeria

Abstract

Honey is a natural sweet substance produced by honey bees. Honey has a very complex chemical composition that varies depending on the botanical source. It has been used both as food and medicine since ancient times. Honey has long been used for treatment of various diseases in folk medicine around the world. The present study was planned to explore the effect of Natural Honey (NH) on the intestinal transit of rats. The rats were fed chow, fresh palm oil diet (FPOD), Thermoxidized Palm Oil Diet (TPOD) and NH; and further the transit point was calculated as a percentage of the total length of the intestine. The NH treated rats significantly decreased the intestinal transit of rats compared to other groups.  The findings exhibited that natural honey used for the treatment of diarrhoea. 

HTML FULL TEXT    PDF    XML 

Estimation of Total Flavonoids and Antioxidant Activity of Spilanthes acmella Leaves 

 

Nelofar Gulam Nabi*, Mukta Shrivastava 

Govt. Maharani Laxmi Bai Girls` P.G. (Autonomous) College, Bhopal (M.P.)-462002, India

Abstract

Flavonoids are a group of polyphenolic compounds, which are widely distributed throughout the plant kingdom. Flavonoids of different classes exhibited various pharmacological and biological activities. The present study was undertaken to investigate the total flavonoids and antioxidant effect of Spilanthes acmella leaves. The ethanol extract of Spilanthes acmella leaves were prepared and performed its phytochemical screening. The total flavonoids and polyphenol were investigated to quantify the presence of polyphenol compounds. The 2,2-diphenyl-1-picryl-hydrazil stable radical (DPPH) and Superoxide scavenging radical were used to determine extract antioxidant activity. The concentrations of flavonoids polyphenol in ethanol extract of Spilanthes acmella were 72.14 QE mg/gm and 84.52 GAE mg/gm, respectively.  The extract exhibited the strongest antioxidant activity, with the lowest IC50 ­value for DPPH and Superoxide scavenging. The IC50 ­value for DPPH and Superoxide scavenging were 134.11 µg/ml and 104.51 µg/ml, respectively.   The strongest antioxidant activity of ethanol extract could be due to the presence of flavonoids and phenols. 

HTML FULL TEXT    PDF    XML 

Quality of Life of Patients with Renal Calculi: An Observational Research

 

R. Ranjith Kumar, Samiha Shah Khan, Md. Mohasin Pasha, Sreenivas Pasula, Bolay Bhattacharya*

 Geethanjali College of Pharmacy, Hyderabad-501301, India

Abstract

Kidney stones are responsible for about 3.66 million medical consults each year with treatment costing about $2 billion annually in medical bills. The main objective of the study was to analyze the quality of life of patients by existing renal calculi. The study would be focused on providing better therapeutic, cost-effective and safe treatment in renal calculi patients. The study was conducted in a urology department of Tulasi Multi-Super Speciality Hospitals (300 bedded hospital), ECIL ‘X’ Road, Hyderabad, India. This study was conducted on 60 patients to study the quality of life of patients with renal calculi for the duration of 6 months. We collected information from patients from 10-80 years of age. For our logical and rational observational study, divided the patient in different age groups, male-female, alcoholic-nonalcoholic, working-nonworking, vegetarian-nonvegetarian, married-unmarried etc. Through our observational study we can reach to a logical conclusion that smoking, alcoholism etc. adversely affects the quality of life of patients of renal calculi. Moreover, vegetarian diet may also indirectly help to improve the quality life of the patients with renal caliculi. Finally, it was found that, if the patient leads hygienic and disciplined life quality of such patients will be somewhat better. If situation permits and open surgery can be avoided by using medicines, modern approach of therapy or modern better surgery, quality of life of patients with renal caliculi will be somewhat better. 

HTML FULL TEXT    PDF    XML 

Pattern of Glucose and Lipid Profile in Obese Diabetic and Non-diabetic Subjects in the Population of Rawalpindi

 

Ahsan Kazmi1, Miss Nadia2, Humaira Zafar3*, Kiran Tauseef Bukhari4, Noor Khan Lakhnana5

1Associate Professor of Chemical Pathology, Al Nafees Medical College & Hospital, Islamabad, Pakistan

2Student of MLT, Rawalpindi Medical College, Rawalpindi, Pakistan

3Associate Professor of Microbiology, Al Nafees Medical College & Hospital, Islamabad, Pakistan

4Assistant Professor of Haematology, Al Nafees Medical College & Hospital, Islamabad, Pakistan

5Professor and Head Department of Pathology, Al Nafees Medical College, Islamabad, Pakistan

Abstract

Obesity is the fifth leading risk for global deaths, which may lead to type 2 diabetes mellitus. This study was planned to see the glucose and lipid profile in obese diabetic and non-diabetic subjects in the local population of Rawalpindi. We planned to study the variation of glucose and lipid profile in obese diabetic and non-diabetic subjects in the local population of Rawalpindi. This case control study was conducted at chemical pathology Laboratory, Holy Family Hospital and Benazir Bhutto Hospital, Rawalpindi. Non-probability purposive sampling was done on 100 subjects out of whom 50 were obese diabetic (21 males and 29 females), and 50 were obese non diabetic (23 males and 27 females) individuals from the general population of Rawalpindi. Blood sample was analyzed for estimation of FPG (fasting plasma glucose) and lipid profile. The t-test was applied and p-Value of 2) and a p-Value is

HTML FULL TEXT    PDF    XML 

Study on Certain Blood and Serum Parameters of Camel Camelus dromedarius Maintained on Different Diets

 

Rakesh Poonia1*, Aakash Srivastava2, Suchitra Sena3, Meera Srivastava1 

1Post-Graduate Department of Zoology, Govt. Dungar College, Bikaner 334001, Rajasthan, India

2SP Medical College, Bikaner, Bikaner 334001, Rajasthan, India

3National Research Centre on Camel, Bikaner, Bikaner 334001, Rajasthan, India

Abstract

Animals including camel (Camelus dromedaries), have been domesticated by man since ancient times especially in Rajasthan. Due to harsh climatic conditions there is often scarcity of grazing pastures in this area and therefore during summers camels are fed roughages and concentrates, as there remains no option to the local farmers. As a result, the proportion of the concentrate and roughage in the complete ration is expected to change the microbial population in the rumen, which in turn is expected to affect their capacity to colonize feed particles and may influence the nutrient utilization from the feed. Cluster bean (guar) belonging to family Leguminosae is one of the most suitable feed in arid areas. Besides, camels are also fed some millet flour or barley flour and gur (molasses) 1g/kg body weight. If this molasses is given in excess amount, it causes gastro-intestinal disorders. Due to introduction of new feed resources, this study was an attempt to investigate certain blood and serum parameters of camels maintained on different diets. An experimental trial was conducted in three groups of camels aged 3-4 years, each group comprising of 4 camels. Three experimental groups were framed Group 1 camels  were fed  guar phalgati (Cyamopsis tetragonaloba) and ground nut (Arachis hypogaea) chara in 1:1 ratio. Group 2 camels were provided ground nut chara alone while, to Group 3 camelsjaggery 50% w/v was administrated orally at the dose 15 g/kg body weight apart from feeding of ground nut chara. The blood samples were collected for hematological, serum biochemical and enzymatic variations. Based on biochemical and enzymatic profile comparison, in the Group 3 camels a significant change in the digestive pattern leading towards acid indigestion was noted. There was an insignificant variation among the enzymatic and biochemical profile of Group 1 and Group 2. From the above blood and serum biochemical and enzymatic changes noticed in different groups fed with different diets, it can be envisaged that there exists a significant role of plan of nutrition on digestive pattern.

HTML FULL TEXT    PDF    XML 

Anti-Microbial Susceptibility Pattern of Linezolid in Various Clinical Isolates

 

Humaira Zafar1*, Naeem Akhtar2, Kiran Tauseef Bukhari3, Noor Khan Lakhnana4 

1Associate Professor, Department of Microbiology, Al Nafees Medical College & Hospital, Islamabad, Pakistan

2Professor and Head Department of Pathology, Rawalpindi Medical College & Allied Teaching Hospitals, Rawalpindi,  Pakistan

3Assistant Professor, Department of Haematology, Al Nafees Medical College & Hospital, Islamabad, Pakistan

4Professor and Head Department of Pathology, Al Nafees Medical College, Islamabad, Pakistan

Abstract

The literature review is suggestive of good efficacy of Linezolid (Oxazolinedione derivative) against gram positive bacteria only. However it is deficient regarding its susceptibility in various clinical isolates. Therefore, the current study was planned to identify the susceptibility pattern of Linezolid in various isolates. Total 748(n) specimens were included in this study. Out of which 144(n) yielded positive growth. For microbiological culture proceedings all recommended CLSI – 2014 (Clinical and laboratory standard institute) guidelines were followed. The linezolid having 30µgm disc potency was used to assess its susceptibility. The clearing zone diameter of >21mm was considered sensitive. Data was recorded and analyzed by using SPSS version 20 for statistical inference. For numerical variables, frequencies were calculated in terms of percentages. The results of current study showed that 84.2% gram-positive and 45.6% gram-negative organisms were sensitive to linezolid. The efficacy of linezolid is more for gram-positive i.e 84.2% as compared to gram-negative 45.6%.

HTML FULL TEXT    PDF    XML 

Effect of Bilateral Oophorectomy and Natural Menopause on Bone Mineral Density

 

Nida H. Ali1, Mayyadah H. Al-Shahlanee1, Abbas M. Jasim2                      

1Dept. of Physiology & Medical Physics, College of Medicine, Al-Mustansiriyah University, Baghdad -14132, Iraq

2Consultant Rheumatologist, Al-Yarmouk Teaching Hospital, Baghdad – 14132, Iraq

Abstract

The objective of this study was to assess the effect of bilateral oophorectomy on bone mineral density in comparison with natural menopause. Bone mineral density (BMD) is  measured with dual energy X-ray DXA of lumber spine and femoral neck in 133 women, aged ranged (45 -70 years). Two surgical groups consist of 100 women either after or before, surgical after menopause SAM women with mean age (66.55 ± 1.11 years), menopause duration mean (15.88 ± 1.19 years) and body mass index BMI mean (32.09 ± 1.37 Kg /m2). Women who underwent surgery before menopause SBM the mean age (57.18 ± 0.84 years), (13.31 ± 0.83 years) the mean of menopause duration and (32.26 ± 0.7 Kg /m2) the mean of body mass index BMI. The natural menopause NM include 33 women mean age (56.45 ± 0.93 years) with (6.24 ± 0.81 years) duration of menopause and (33.49 ± 1.08 Kg /m2) BMI. The mean of BMD and T-score in lumber spine L1-L4 in SAM group was (0.84 ± 0.03 gr/cm2 and -2.32 ± 0.25) respectively, in the SBM group (BMD = 0.82 ± 0.01 gr/cm2 and T-score -2.46 ± 0.12) comparing to natural menopause group NM (BMD = 1.16 ± 0.03 gr /cm2 and T-score 0.31 ± 0.23). The mean of BMD measured for femoral neck in SAM (0.72± 0.03 gr /cm2 and T-score = - 1.54 ± 0.2), in SBM (BMD = 0.81 ± 0.81 gr/cm2 and T-score = - 0.86 ± 0.12), in NM (BMD = 0.93 ± 0.03 gr/cm2 and T-score = 0.3 6 ± 0.03). Bilateral oophorectomy associated with decrease in BMD, in addition age and duration of menopause are important factors affected on BMD.

HTML FULL TEXT    PDF    XML